Assay Detail
Binding
CHEMBL933759
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Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Diphenidol-related diamines as novel muscarinic M4 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.82 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59898 | — | — | 1 | 8.19 |
| CHEMBL402207 | — | — | 1 | 7.90 |
| CHEMBL403773 | — | — | 1 | 7.13 |
| CHEMBL254586 | — | — | 1 | 6.54 |
| CHEMBL256923 | — | — | 1 | 6.21 |
| CHEMBL1529 | DIPHENIDOL HYDROCHLORIDE | 4.0 | 1 | 6.04 |
| CHEMBL257174 | — | — | 1 | 5.93 |
| CHEMBL258385 | — | — | 1 | 5.93 |
| CHEMBL402282 | — | — | 1 | 5.91 |
| CHEMBL257804 | — | — | 1 | 5.57 |
| CHEMBL436850 | — | — | 1 | 5.32 |
| CHEMBL258161 | — | — | 1 | 5.01 |
| CHEMBL257586 | — | — | 1 | 4.95 |
| CHEMBL403592 | — | — | 1 | 4.95 |
| CHEMBL404866 | — | — | 1 | 4.65 |
| CHEMBL257547 | — | — | 1 | 4.64 |
| CHEMBL403029 | — | — | 1 | 4.00 |
| CHEMBL255692 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59898 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL402207 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL403773 | — | Ki | = | 74.13 | nM | 7.13 |
| CHEMBL254586 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL256923 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL1529 | DIPHENIDOL HYDROCHLORIDE | Ki | = | 912.01 | nM | 6.04 |
| CHEMBL257174 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL258385 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL402282 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL257804 | — | Ki | = | 2691.53 | nM | 5.57 |
| CHEMBL436850 | — | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL258161 | — | Ki | = | 9772.37 | nM | 5.01 |
| CHEMBL257586 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL403592 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL404866 | — | Ki | = | 22387.21 | nM | 4.65 |
| CHEMBL257547 | — | Ki | = | 22908.68 | nM | 4.64 |
| CHEMBL403029 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL255692 | — | Ki | = | 162181.01 | nM | - |